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Title

Evidence for distinct antagonist-revealed functional states of 5-hydroxytryptamine(2A) receptor homodimers

AuthorsVilaró, Maria Teresa ; Mengod Los Arcos, Guadalupe ; Loza, María Isabel
Issue Date11-Mar-2009
PublisherAmerican Society for Pharmacology and Experimental Therapeutics
CitationMolecular Pharmacology 75(6): 1380-1391 (2009)
AbstractThe serotonin (5-hydroxytryptamine; 5-HT) 2A receptor is a cell surface class A G protein-coupled receptor that regulates a multitude of physiological functions of the body and is a target for antipsychotic drugs. Here we found by means of fluorescence resonance energy transfer and immunoprecipitation studies that the 5-HT2A -receptor homodimerized in live cells, which we linked with its antagonist-dependent fingerprint in both binding and receptor signaling. Some antagonists, like the atypical antipsychotics clozapine and risperidone, differentiate themselves from others, like the typical antipsychotic haloperidol, antagonizing these 5-HT2A receptor-mediated functions in a pathway-specific manner, explained here by a new model of multiple active interconvertible conformations at dimeric receptors.
Descriptionet al.
Publisher version (URL)http://dx.doi.org/10.1124/mol.108.054395
URIhttp://hdl.handle.net/10261/31994
DOI10.1124/mol.108.054395
ISSN0026-895X
E-ISSN1521-0111
Appears in Collections:(IIBB) Artículos
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